Abstract: Described herein is a dichloroacetic acid conjugating diphenyl ethane compound, and a preparation method and an application thereof. The dichloroacetic acid conjugating diphenyl ethane compound has a stable structure, low toxicity, a simple preparation process and a high yield, without necessity to preserve it in a dark place, and has anti-tumor activity against a variety of tumor cells cultured in vitro, and the anti-tumor effect in vivo.